integrase (in)

Raltegravir potassium (MK 0518 potassium salt) 是一种整合酶抑制剂，用于研究 HIV 感染。

HIV-1integrase inhibitor 10 是一种 HIV-1变构整合酶抑制剂 (ALLINI)，具有口服活性。HIV-1integrase inhibitor 10 可抑制 NLRepRluc 病毒在 MT-2 细胞中的生长，其 EC50值为 3-5 nM。HIV-1integrase inhibitor 10 可用于人类免疫缺陷病毒-1 (HIV-1) 的研究。

HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor (IC50: 33.3 nM).

Hiv-1 integrase inhibitor is an effective anti-HIV drug.

HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 2.7 nM).

HIV-1 integrase inhibitor 4 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 3.7 nM).

HIV-1integrase inhibitor 11 (compound 5) 作为一种HIV-1整合酶的抑制剂，显示出了显著的生物活性，其IC50值为 125 μM。

Integrase-LEDGF p75 allosteric inhibitor 1 是一种口服具有活力的 integrase-LEDGF p75 (IN-LEDGF p75) 变构抑制剂。Integrase-LEDGF p75 allosteric inhibitor 1 能够抑制 HIV-1 DNA 整合，表现出抗病毒作用，能够作用于 HIV-1重组分子克隆 NL432 (EC50: 3.9 nM)。

HIV-1 integrase inhibitor 9 (compound 8a) 是一种 HIV-1 RNase H 的有效抑制剂 (IC50: 12.3 μM)，具有抗病毒作用。

HIV-1 integrase inhibitor 8 是一种 HIV-1 整合酶抑制剂，整合是HIV 复制的必要步骤。

Bis-T-23是一种肌动蛋白依赖性达纳敏低聚物的促进剂，是一种 HIV-I 整合酶抑制剂，是泰尔普斯丁衍生物。Bis-T-23可以促进肌动蛋白依赖性的dynamin 寡聚化。Bis-T-23可用于HIV 和慢性肾脏疾病（CKD）的研究。

Pirmitegravir (STP0404) 是一种针对 LEDGF p75 结合位点的异位整合酶（ALLINI）的强效选择性抑制剂。 Pirmitegravir 可抑制 PBMC。 Pirmitegravir 具有显著的抗病毒活性，可用于研究 HIV 病毒感染。

MK-2048是HIV 整合酶和INR263K 的抑制剂，IC50分别为2.6 nM 和1.5 nM。

GSK-364735 是一种人类免疫缺陷病毒 1 型整合酶（HIV-1 IN） 抑制剂，具有抗病毒活性，可用于研究逆转录病毒感染。

Raltegravir (MK-0518) 是一种HIV 整合酶抑制剂。

L-Chicoric Acid (trans-Caffeoyltartaric acid) 是一种二咖啡酰酒石酸，是一种选择性可逆的 HIV-1 整合酶抑制剂，IC50约为 100 nM。它还可抑制 HIV-1 复制。

Cichoric Acid (Dicaffeoyltartaric acid) 是一种天然化合物，具有抗氧化作用。

Equisetin, an N-methylserine-derived acyl tetramic acid isolated from the terrestrial fungus Fusarium equiseti NRRL 5537, functions as a Quorum-sensing inhibitor (QSI) that specifically attenuates QS-regulated virulence phenotypes in P. aeruginosa, presenting a potent lead for treating P. aeruginosa infections without hindering bacterial growth. This tetramate-containing natural product possesses antibiotic and cytotoxic properties, effectively inhibiting the growth of Gram-positive bacteria and HIV-1 integrase activity, yet it does not impact Gram-negative bacteria.

(±)-BI-D is an effective ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site (IC50: 2.4–2.9 μM).

BMIM-TFSI (化合物 8) 是HIV-1整合酶的抑制剂，能高效抑制整合反应中的3'-processing (3'-P) 和 strand transfer (ST) 两个步骤，适用于HIV-1研究。

L 870810 is a small-molecule inhibitor of HIV-1 integrase with potent antiviral activity in cell culture and good pharmacokinetic properties.

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544(2019) 2.Reese, M.J., Savina, P.M., Generaux, G.T., et al.In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitorDrug Metab. Dispos.41(2)353-361(2013)